Search Result

Results for "

methyltransferase+inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Apoptosis (11) Autophagy (5) Bacterial (3) Caspase (2) CD38 (1) CD44 (1) Cholecystokinin Receptor (1) COMT (3) COX (5) CRFR (2) Dengue Virus (1) DNA Methyltransferase (14) Endogenous Metabolite (2) Ferroportin (1) Fungal (1) Histone Methyltransferase (31) Integrin (1) Interleukin Related (1) Isotope-Labeled Compounds (6) Keap1-Nrf2 (1) Mitochondrial Metabolism (1) MMP (1) NF-κB (1) NO Synthase (5) Nuclear Hormone Receptor 4A/NR4A (7) Nucleoside Antimetabolite/Analog (3) Parasite (8) PGE synthase (5) Reactive Oxygen Species (ROS) (6) Reference Standards (10) SARS-CoV (1) Sirtuin (1) TNF Receptor (1) Vasopressin Receptor (1) Virus Protease (1) WDR5 (4)
By Research Areas:	Cancer (38) Cardiovascular Disease (6) Endocrinology (1) Infection (17) Inflammation/Immunology (16) Metabolic Disease (2) Neurological Disease (15)

By Targets:

Adrenergic Receptor (1)

Apoptosis (11)

Autophagy (5)

Bacterial (3)

Caspase (2)

CD38 (1)

CD44 (1)

Cholecystokinin Receptor (1)

COMT (3)

COX (5)

CRFR (2)

Dengue Virus (1)

DNA Methyltransferase (14)

Endogenous Metabolite (2)

Ferroportin (1)

Fungal (1)

Histone Methyltransferase (31)

Integrin (1)

Interleukin Related (1)

Isotope-Labeled Compounds (6)

Keap1-Nrf2 (1)

Mitochondrial Metabolism (1)

MMP (1)

NF-κB (1)

NO Synthase (5)

Nuclear Hormone Receptor 4A/NR4A (7)

Nucleoside Antimetabolite/Analog (3)

Parasite (8)

PGE synthase (5)

Reactive Oxygen Species (ROS) (6)

Reference Standards (10)

SARS-CoV (1)

Sirtuin (1)

TNF Receptor (1)

Vasopressin Receptor (1)

Virus Protease (1)

WDR5 (4)

By Research Areas:

Cancer (38)

Cardiovascular Disease (6)

Endocrinology (1)

Infection (17)

Inflammation/Immunology (16)

Metabolic Disease (2)

Neurological Disease (15)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0004

Decitabine Maximum Cited Publications 168 Publications Verification 5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716	DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog	Cancer
Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .

HY-15593

Pinometostat 25+ Cited Publications EPZ-5676	Histone Methyltransferase	Cancer
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

HY-B0464

Hydralazine hydrochloride 3 Publications Verification	PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX	Cardiovascular Disease Inflammation/Immunology Cancer
Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-134124

*Glutathione ethyl* ester**	Reactive Oxygen Species (ROS)	Metabolic Disease
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .

HY-B1322

Amodiaquine dihydrochloride dihydrate 10+ Cited Publications Amodiaquin dihydrochloride dihydrate	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-154812

Gintemetostat KTX-1001	Histone Methyltransferase CD44	Cancer
Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC₅₀ values ranging 0.460-2.17 nM and NSD2 SET domain IC₅₀ of 2.32 nM and K_d values ranging 6.3-70.4 nM .Gintemetostat reduces H₃K₃₆me₂ levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma .

HY-112445

SGC3027 5+ Cited Publications	Histone Methyltransferase	Cancer
SGC3027 is a histone methyltransferase inhibitor . SGC3027 is the first potent, selective and cell active chemical probe for PRMT7 .

HY-B1322A

Amodiaquine 10+ Cited Publications Amodiaquin	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-10587

BIX-01294 25+ Cited Publications	Histone Methyltransferase Autophagy	Cancer
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC₅₀s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells .

HY-13420

Zebularine 5 Publications Verification NSC309132; 4-Deoxyuridine	DNA Methyltransferase Autophagy	Cancer
Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor. Zebularine also inhibits cytidine deaminase with a K_i of 0.95 μM.

HY-P10272

Rusfertide PTG-300	Ferroportin	Others
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .

HY-12220

MM-102 4 Publications Verification HMTase Inhibitor IX	WDR5 Apoptosis NF-κB TNF Receptor Interleukin Related	Inflammation/Immunology Cancer
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC₅₀=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .

HY-A0248A

Polymyxin B1 1 Publications Verification	Bacterial	Infection
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-B1322B

Amodiaquine dihydrochloride 10+ Cited Publications Amodiaquin dihydrochloride	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a K_i of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-P1108A

Astressin 2B TFA 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-P1108

Astressin 2B 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-141429A

AS-99 TFA 2 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 μM, K_d= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-148458

EZH2-IN-14	Histone Methyltransferase	Cancer
EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .

HY-B0464A

Hydralazine 3 Publications Verification	DNA Methyltransferase Reactive Oxygen Species (ROS) COX NO Synthase PGE synthase	Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-A0004R

Decitabine (Standard) 5-Aza-2'-deoxycytidine (Standard); 5-AZA-CdR (Standard); NSC 127716 (Standard)	Reference Standards DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog	Cancer
Decitabine (Standard) is the analytical standard of Decitabine. This product is intended for research and analytical applications. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .

HY-108239

BIX-01294 trihydrochloride 25+ Cited Publications	Histone Methyltransferase Autophagy	Cancer
BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC₅₀s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells .

HY-12991A

BIX-01338 hydrate	Histone Methyltransferase	Cancer
BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.

HY-100846

JQEZ5 3 Publications Verification	Histone Methyltransferase	Cancer
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC₅₀ of 80 nM. JQEZ5 has anti-tumor effects .

HY-19554A

MM-401 TFA 1 Publications Verification	WDR5 Apoptosis	Cancer
MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC₅₀ = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .

HY-114209

MRK-740 2 Publications Verification	Histone Methyltransferase	Cancer
MRK-740, a chemical probe, is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC₅₀ of 80?nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC₅₀?=?0.8?μM) .

HY-119390

AA-CW236	DNA Methyltransferase	Cancer
AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification .

HY-100959

3,5-Dinitrocatechol OR-486; 3,5-Dinitropyrocatechol	COMT	Neurological Disease
3,5-Dinitrocatechol (OR-486) is a potent *catechol-O-methyltransferase* inhibitor, with an IC₅₀ of 12 nM. 3,5-Dinitrocatechol can be used in the preparation of the molybdenum (VI)- 3,5-Dinitrocatechol complex .

HY-141430

AS-85	Histone Methyltransferase	Cancer
AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC₅₀=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the K_d value of 0.78 μM .

HY-100967

SKF 91488 dihydrochloride Homodimaprit dihydrochloride	Histone Methyltransferase	Infection Cardiovascular Disease Inflammation/Immunology
SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a K_i value of 0.9 μM. SKF 91488 dihydrochloride can block histamine metabolism and increase histamine concentrations. SKF 91488 dihydrochloride can increase blood pressure and enhance bronchoconstriction. SKF 91488 can be used for the researches of infection, inflammation and cardiovascular disease, such as Mycoplasma pneumonia and hemorrhagic hypotension .

HY-19554

MM-401	WDR5 Apoptosis	Cancer
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC₅₀ = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .

HY-P10143

MMP-2/MMP-9 Substrate Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt	MMP	Others
MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties .

HY-A0248AS

Polymyxin B1-d7 TFA	Isotope-Labeled Compounds Bacterial	Infection
Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-141429

AS-99 free base 2 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-B1322R

Amodiaquine dihydrochloride dihydrate (Standard) Amodiaquin dihydrochloride dihydrate (Standard)	Nuclear Hormone Receptor 4A/NR4A Reference Standards Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-B0464S1

Hydralazine-d5 hydrochloride	Isotope-Labeled Compounds PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX	Cancer
Hydralazine-d₅ (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-P10563

Noraramtide BHV-1100	CD38	Cancer
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .

HY-122936

Tanshindiol C	Histone Methyltransferase Keap1-Nrf2 Sirtuin	Cardiovascular Disease Cancer
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .

HY-P3066

SKF 100398 d(CH2)5Tyr(Et)VAVP	Vasopressin Receptor	Metabolic Disease
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .

HY-B0464S

Hydralazine-d4 hydrochloride	Isotope-Labeled Compounds PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX	Cardiovascular Disease
Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-P10828

MAPI	Virus Protease	Infection Inflammation/Immunology
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .

HY-141429C

AS-99	Histone Methyltransferase Apoptosis	Cancer
AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 μM, K_d= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-B1322AS

Amodiaquine-d10	Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine-d₁₀ is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-176820

MRK-740-NC	Histone Methyltransferase	Cancer
MRK-740-NC is a PRDM7/9 histone methyltransferase inhibitor. MRK-740-NC is a negative control compound of MRK-740 (HY-114209). MRK-740-NC has no inhibitory activity for PRDM7 and PRDM9 by replacing the methyl pyridine moiety of MRK-740 by a phenyl group .

HY-B1322AR

Amodiaquine (Standard) Amodiaquin (Standard)	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Reference Standards	Infection Neurological Disease Inflammation/Immunology
Amodiaquine (Standard) is the analytical standard of Amodiaquine. This product is intended for research and analytical applications. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .

HY-135043

S-Aristeromycinyl-L-homocysteine	DNA Methyltransferase	Others
S-Aristeromycinyl-L-homocysteine is an S-adenosylmethionine-dependent methyltransferase inhibitor .

HY-15593R

Pinometostat (Standard) EPZ-5676 (Standard)	Histone Methyltransferase Reference Standards	Cancer
Pinometostat (Standard) is the analytical standard of Pinometostat. This product is intended for research and analytical applications. Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

HY-139137

N-Acetyl-S-geranylgeranyl-L-cysteine AGGC	DNA Methyltransferase Integrin	Cancer
N-Acetyl-S-geranylgeranyl-L-cysteine is a *Methyltransferase* inhibitor. N-Acetyl-S-geranylgeranyl-L-cysteine inhibits beta 2 integrin-induced actin polymerization with an IC₅₀ of 45 nM .

HY-19061

CGP 28014	COMT	Neurological Disease
CGP 28014 is a *catechol-O-methyltransferase* inhibitor. CGP 28014 can lower HVA levels and increase DOPAC levels in the striatum of rats, making it useful for research on Parkinson's disease .

HY-145950

2′-Deoxy-5-nitrocytidine	DNA Methyltransferase	Cancer
2′-Deoxy-5-nitrocytidine is a DNA Methyltransferase inhibitor extracted from patent CN108498529A. 2′-Deoxy-5-nitrocytidine can be used for the research of cancer .

HY-163631

Antibacterial agent 218	Fungal Endogenous Metabolite	Infection
Antibacterial agent 218 (compound d28) is an orally active sterol 24-C-Methyltransferase inhibitor with the IC₅₀ of 0.273 μM. Antibacterial agent 218 shows antifungal activity against the C.albicans SC5314 with the IC₅₀ of 0.25 μg/mL .

Cat. No.	Product Name	Target	Research Area

HY-134124

*Glutathione ethyl* ester**	Reactive Oxygen Species (ROS)	Metabolic Disease
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .

HY-P10272

Rusfertide PTG-300	Ferroportin	Others
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .

HY-A0248A

Polymyxin B1 1 Publications Verification	Bacterial	Infection
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-P1108A

Astressin 2B TFA 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-P1108

Astressin 2B 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-19554

MM-401	WDR5 Apoptosis	Cancer
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC₅₀ = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .

HY-P10143

MMP-2/MMP-9 Substrate Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt	MMP	Others
MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties .

HY-A0248AS

Polymyxin B1-d7 TFA	Isotope-Labeled Compounds Bacterial	Infection
Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-P10563

Noraramtide BHV-1100	CD38	Cancer
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .

HY-P3066

SKF 100398 d(CH2)5Tyr(Et)VAVP	Vasopressin Receptor	Metabolic Disease
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .

HY-P10828

MAPI	Virus Protease	Infection Inflammation/Immunology
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .

HY-P4756

*N-(2-Carbamoyl-ethyl)-Val-Leu-anilide*	Peptides	Others
N-(2-Carbamoyl-ethyl)-Val-Leu-anilide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .

HY-P2592

Ro 23-7014	Cholecystokinin Receptor	Others
Ro 23-7014 is an appetite suppressant. Ro 23-7014 is an analog of cholecystokinin (CCK-7) .

HY-125628

Kahalalide A	Endogenous Metabolite	Infection
Kahalalide A is an anti-mycobacterial compound with antimicrobial activity. Kahalalide A is derived from the marine mollusk Elysia rufescens. Kahalalide A has attracted extensive attention in natural product research due to its potential medicinal value .

HY-A0248AS1

Polymyxin B1-D-Leu-d7 TFA	Isotope-Labeled Compounds Bacterial	Infection
Polymyxin B1-D-Leu-d₇ TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-A0248A

Polymyxin B1 1 Publications Verification	Infection Microorganisms Classification of Application Fields Antibiotics Antibacterial Disease Research Disease Research Fields Other Antibiotics Source Classification	Bacterial
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-A0248AS

Polymyxin B1-d7 TFA	Structural Classification Microorganisms Antibiotics Antibacterial Disease Research Other Antibiotics Source Classification	Isotope-Labeled Compounds Bacterial
Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-122936

Tanshindiol C	Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants	Histone Methyltransferase Keap1-Nrf2 Sirtuin
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .

HY-N14558

3',8-Dihydroxy-4',6,7-trimethoxyisoflavone	Microorganisms Antibiotics Other Antibiotics Source Classification	Others
3',8-Dihydroxy-4',6,7-trimethoxyisoflavone is found in the strain of Streptomyces sp. 3',8-Dihydroxy-4',6,7-trimethoxyisoflavone is a catechole-O-methyltransferase inhibitor (IC₅₀ is 0.2 g/mL) .

HY-A0248AS1

Polymyxin B1-D-Leu-d7 TFA	Structural Classification Microorganisms Antibiotics Antibacterial Disease Research Other Antibiotics Source Classification	Isotope-Labeled Compounds Bacterial
Polymyxin B1-D-Leu-d₇ TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

Cat. No.	Product Name	Chemical Structure

HY-A0248AS

Polymyxin B1-d7 TFA

Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-B0464S1

Hydralazine-d5 hydrochloride

Hydralazine-d₅ (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-B0464S

Hydralazine-d4 hydrochloride

Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-B1322AS

Amodiaquine-d10
Amodiaquine-d₁₀ is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-B1322AS1

Amodiaquine-d10 hydrochloride
Amodiaquine-d₁₀ hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-A0004S

Decitabine-13C5

Decitabine- ¹³C₅ (5-Aza-2'-deoxycytidine- ¹³C₅) is ¹³C labeled Decitabine. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .

HY-A0248AS1

Polymyxin B1-D-Leu-d7 TFA

Polymyxin B1-D-Leu-d₇ TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

methyltransferase+inhibitor

Inhibitors & Agonists

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
Products